Related Products of 851759-19-8 ,Some common heterocyclic compound, 851759-19-8, molecular formula is C8H8ClNO2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
To a solution of tert-butyl 2,2-dimethyl-3-oxo-piperazine-1-carboxylate (1.60 g, 7.01 mmol) in DMF (10 mL) is added 60% NaH/mineral (280 mg, 7.00 mmol). The mixture is stirred at rt for 20 mm, till the bubbling subsided. Then to it are added TBAI (70 mg, 0.19 mmol) and tertbutyl 2,2-dimethyl-3-oxo-piperazine-1-carboxylate (1.6 g, 7.1 mmol). The mixture is stirred at rt for lh under nitrogen, LC-MS of the crude shows a littlew conversion. Then the temperature is raised to 60C, stirred for 3h. After cooling to rt, the mixture is neutralized with formic acid, diluted with Et0Ac (80 mL), washed with water and brine consecutively, dried over sodium sulfate, filtered. The filtrate is concentrated to dryness under reduced pressure and the residue is purified on Biotage SNAP 50g silica gel cartridge eluting with Et0Ac/hexanes 0-30% in 2OCV to obtain tert-butyl 4-(5-methoxycarbonyl-6-methyl-2-pyridyl )-2,2-dimethyl-3-oxo-piperazine-1- carboxylate (755 mg, 37%) as a yellowish solid. LC-MS: 378.77 M(+H+), calc. 378.2028. RT: 1.9 mm using Method C.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,851759-19-8, its application will become more common.
Reference:
Patent; VERTEX PHARMACEUTICALS INCORPORATED; LIU, Bingcan; DORICH, Stephane; DE LESELEUC, Mylene; DUPONT-GAUDET, Kristina; JAMES, Clint, Alwyn; VAILLANCOURT, Louis; BEAULIEU, Marc-Andre; STURINO, Claudio; (236 pag.)WO2018/57588; (2018); A1;,
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